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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS. Cheung M, et al. Among authors: willette rn. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523109 Free PMC article.
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Washburn DG, Holt DA, Dodson J, McAtee JJ, Terrell LR, Barton L, Manns S, Waszkiewicz A, Pritchard C, Gillie DJ, Morrow DM, Davenport EA, Lozinskaya IM, Guss J, Basilla JB, Negron LK, Klein M, Willette RN, Fries RE, Jensen TC, Xu X, Schnackenberg CG, Marino JP Jr. Washburn DG, et al. Among authors: willette rn. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4979-84. doi: 10.1016/j.bmcl.2013.06.047. Epub 2013 Jun 26. Bioorg Med Chem Lett. 2013. PMID: 23886683
Toward improved myocardial maturity in an organ-on-chip platform with immature cardiac myocytes.
Sheehy SP, Grosberg A, Qin P, Behm DJ, Ferrier JP, Eagleson MA, Nesmith AP, Krull D, Falls JG, Campbell PH, McCain ML, Willette RN, Hu E, Parker KK. Sheehy SP, et al. Among authors: willette rn. Exp Biol Med (Maywood). 2017 Nov;242(17):1643-1656. doi: 10.1177/1535370217701006. Epub 2017 Mar 26. Exp Biol Med (Maywood). 2017. PMID: 28343439 Free PMC article.
Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2.
Willette RN, Bao W, Nerurkar S, Yue TL, Doe CP, Stankus G, Turner GH, Ju H, Thomas H, Fishman CE, Sulpizio A, Behm DJ, Hoffman S, Lin Z, Lozinskaya I, Casillas LN, Lin M, Trout RE, Votta BJ, Thorneloe K, Lashinger ES, Figueroa DJ, Marquis R, Xu X. Willette RN, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):443-52. doi: 10.1124/jpet.107.134551. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499744
146 results